21070-54-2

Upstream product

• 99-91-2 para-chloroacetophenone 
• 50-00-0 formaldehyd 
• 506-59-2 N,N-dimethylammonium chloride 
• 593-51-1 methylamine hydrochloride 

Downstream Products

• 128258-27-5 3-Methyl-butyric acid 3-(4-chloro-benzoyl)-4-(4-chloro-phenyl)-1-methyl-piperidin-4-yl ester 
• 128258-25-3 Butyric acid 3-(4-chloro-benzoyl)-4-(4-chloro-phenyl)-1-methyl-piperidin-4-yl ester 
• 18164-92-6 Acetic acid 3-(4-chloro-benzoyl)-4-(4-chloro-phenyl)-1-methyl-piperidin-4-yl ester 
• 128258-23-1 Propionic acid 3-(4-chloro-benzoyl)-4-(4-chloro-phenyl)-1-methyl-piperidin-4-yl ester 
• 128257-96-5 Methanesulfonate₃-(4-chloro-benzoyl)-4-(4-chloro-phenyl)-4-hydroxy-1,1-dimethyl-piperidinium; 

Relevant academic research and scientific papers

Synthesis and evaluation of anticonvulsant activities of some bis Mannich bases and corresponding piperidinols

Some acetophenone derived bis Mannich bases (B1-B5) and piperidinols (C1, C4), which are the structural isomers of B1 and B4, and also quaternary piperidine derivative C6 were synthesized and studied for anticonvulsant activity. Of the compounds, C6 was reported for the first time. Chemical structures of the compounds were confirmed by UV, IR, 1H-NMR, 13C-NMR, mass spectra and elemental analysis. Their anticonvulsant activities were determined by maximal electroshock (MES), subcutaneous metrazol (scMet) tests and rotarod test for neurological deficits. According to the activity studies, B2, B4, C1 and C4 derivatives were found to be protective against MES at 30 mg/kg and above. B1, B2, B3, B4, C4 and C6 derivatives were found to be protective against scMet, at different dose levels ranging from 30 to 300 mg/kg. Since no neurotoxicity was detected for the compounds B4 and C4, they seem to be candidate compounds for further synthesis and in vivo studies for their potential anticonvulsant activity.

Molecular modeling, structure-activity relationships and functional antagonism studies of 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketones as a novel class of dopamine transporter inhibitors

We previously disclosed the discovery of 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone (3) as a novel class of dopamine transporter (DAT) inhibitors and showed that (±)-3 has a significant functional antagonism against cocaine in vitro. Our previous preliminary structure-activity relationship study led to identification of a more potent DAT inhibitor [(±)-4] but this compound failed to show any significant functional antagonism. To search for more potent analogues than 3 but still displaying significant functional antagonism, further SARs, molecular modeling studies and in vitro pharmacological evaluation of this novel class of DAT inhibitors were performed. Sixteen new analogues were synthesized in racemic form and evaluated as DAT inhibitors. It was found that seven new analogues are reasonably potent DAT inhibitors with Ki values of 0.041-0.30 and 0.052-0.16μM in [3H]mazindol binding and inhibition of DA reuptake. Chiral isomers of several potent DAT inhibitors were obtained through chiral HPLC separation and evaluated as inhibitors at all the three monoamine transporter sites. In general, the (-)- isomer is more active than the (+)-isomer in inhibition of DA reuptake and all the (-)-isomers are selective inhibitors at the DAT site. Evaluation of cocaine's effect on dopamine uptake in the presence and absence of (+)-3 and (-)-3 showed that (-)-3 is responsible for the functional antagonism obtained with the origin lead (±)-3 in binding and inhibition of DA reuptake, appeared to have improved functional antagonism as compared to (±)-3. Copyright

Synthesis and preliminary study of some ring-substituted arylpropanonoamines and their quaternary salts

The synthesis and biological examination of 1-phenyl- and 1-(4-bromophenyl)-3-(N-2-hydroxyethyl-N-methylamino) propan-1-one methiodides and 1-(4-bromophenyl)-3-(N-2-hydroxyethyl-N-methylamino)propan-1-ol methiodide as model potential intravenous anestheti